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BAY 61-3606 dihydrochloride

CAS No. : 648903-57-5

MCE 站：BAY 61-3606 dihydrochloride

产品活性：BAY 61-3606 dihydrochloride 是一种口服有效的，ATP 竞争性的，可逆的选择性 Syk 抑制剂，K_i 为 7.5 nM，IC₅₀ 为 10 nM。BAY 61-3606 dihydrochloride 降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化。BAY 61-3606 dihydrochloride 降低 K-rn 细胞裂解物中 Syk 磷酸化。Bay 61-3606 dihydrochloride 作用于乳腺癌细胞，通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：Syk  |  Apoptosis

In Vitro: BAY 61-3606 (0.01-10 μM ; 48 hours) significantly reduces the cell viability of SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells in a dose-dependent matter. SH-SY5Y cells expressing high SYK levels are significantly more sensitive to BAY 61-3606 in comparison to SK-N-BEcells expressing very low or no SYK.
BAY 61-3606 (0.4 and 0.8 μM; 4 or 24 hours) inhibits SYK activity by reducing ERK1/2 and Akt phosphorylation in neuroblastoma cell SH-SY5Y.
BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation in K-rn cell lysates.

In Vivo: Bay 61-3606 (50 mg/kg; administered twice a week for two weeks by intraperitoneal injection) alone leads to more efficacious reductions than that of TNF-related apoptosis-inducing ligand (TRAIL; 10 mg/kg) alone in MCF-7 tumor xenograft-bearing BALB/c nude mice. Bay 61-3606 administered in TRAIL combination significantly reduces the volume of the xenografted tumor.

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